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Belizatinib (TSR-011) is an orally available, potent small molecule inhibitor targeting both the receptor tyrosine kinase anaplastic lymphoma kinase (ALK) and the tropomyosin-related kinases TRKA, TRKB, and TRKC. It was developed as a potential antineoplastic agent for cancers driven by ALK or NTRK gene rearrangements, such as non-small cell lung cancer (NSCLC). Belizatinib binds to and inhibits ALK and TRK kinases, disrupting their signaling pathways and impeding tumor cell growth in tumors overexpressing these targets. Clinical trials demonstrated activity in patients with relapsed or refractory ALK- or TRK-positive advanced cancers, including those resistant to prior ALK inhibitors. However, development of belizatinib was discontinued due to limited clinical activity compared to other agents in this class[1][3][5][6][8].
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